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首页-小分子抑制剂&激动剂-Others-Other Targets-BAY 2402234
BAY 2402234

Chemical Structure : BAY 2402234

CAS No.: 2225819-06-5

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BAY 2402234 (Orludodstat, BAY2402234, BAY-2402234)

货号: PC-36161Not For Human Use, Lab Use Only.

BAY 2402234 (BAY2402234) is a novel potent, selective, orally bioavailable DHODH inhibitor with IC50 of 1.2 nM (human full-length DHODH).

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1 mg ￥1280 In stock
5 mg ￥2780 In stock
10 mg ￥4580 In stock
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纯度 & COA & 质检文件 纯度: 99.45% (HPLC) Select Batch:

生物&药学活性

Orludodstat (BAY2402234) is a novel potent, selective, orally bioavailable DHODH inhibitor with IC50 of 1.2 nM (human full-length DHODH).
BAY2402234 binds the ubiquinone binding site of DHODH between the N-terminal helices.
BAY2402234 causes dose-dependent upregulation of CD11b with EC50s of 3.16 nM in MOLM-13 cells and 0.96 nM in HEL cells, inhibits the proliferation of THP-1 cells with an IC50 of 2.6 nM, as well as nine other leukemia cell lines representing diverse AML subtypes (IC50=0.08-8.2 nM).
BAY 2402234 shows monotherapy efficacy and differentiation induction across multiple AML subtypes both in vitro and in vivo.

物理化学性质&存储条件

分子量 520.841
分子式 C21H18ClF5N4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-N-(2-chloro-6-fluorophenyl)-4-(4-ethyl-3-(hydroxymethyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)-5-fluoro-2-((1,1,1-trifluoropropan-2-yl)oxy)benzamide

参考文献

1. Christian S, et al. Leukemia. 2019 Apr 2. doi: 10.1038/s41375-019-0461-5.

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